1. Field of the Invention
The present invention relates to N-heteroaryl-N'-phenylurea derivatives or pharmacologically acceptable salts thereof, which have inhibitory effect on acyl-CoA:cholesterol O-acyltransferase (ACAT).
The compounds of the present invention have the effect of reducing serum cholesterol by inhibiting the absorption of cholesterol from intestinal tract and suppress the accumulation of cholesterol esters in the arterial wall. Therefore, they are useful as a prophylactic and therapeutic agent for hypercholesterolemia, atherosclerosis and various diseases caused by them (for example, ischemic heart diseases such as myocardial infarction, and cerebrovascular diseases such as cerebral infarction and cerebral apoplexy).
2. Related Art
As to N-heteroaryl-N'-phenylurea derivatives, there are the following disclosures.
Japanese Patent Unexamined Publication No. 3-7259 discloses that N-quinoline-N'-phenylurea derivatives represented by the formula (A): ##STR2## (wherein the ring A, ring B and ring C may have a substituent, and each of m and n is zero or an integer of 1) have ACAT-inhibitory activity. Japanese Patent Unexamined Publication No. 3-223254 discloses that N-quinoline-N'-phenylurea derivatives represented by the formula (B): ##STR3## (wherein the ring A', ring B and ring C' may have a substituent, n is zero or an integer of 1, and X' is ##STR4## have ACAT-inhibitory activity.
J. Ind. Chem. Soc., 1978, 55(9), 910-913 discloses that compounds having, like the compounds of the present invention, a benzofuran skeleton which are represented by the formula (C): ##STR5## (wherein Re is a hydrogen atom or a methyl group) have antimicrobial activity, antibacterial activity, antiparasitic activity and anti-amoeba activity.
Farmaco, Ed. Sci. 1979, 34(6), 507-517 describes compounds having an indole skeleton which are represented by the formula (D): ##STR6## but it does not describes them as having ACAT-inhibitory activity.